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Trazodone
drug data and news
Trazodone drug data, resources, and news articles (when available). Onconews.org provides news on cancer research. This section, which includes profiles on medicines that may or not be cancer-related is in beta form. If things run smoothly we will be releasing a new format late in the summer of 2006.
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| Generic name | Trazodone | ||
| Brand Names/Synonyms | Trazodonum [Latin]; AF-1161; Beneficat; Bimaran; CHEMBANK850; Desirel; Desyrel; Molipaxin; Pragmazone; Sideril; T137; T6154; Thombran; Tombran; Trazalon; Trazodil; Trazodon; Trazodona [Inn-Spanish]; Trazodona [Spanish]; Trazodone; Trazodone Hcl; Trazodone Hydrochloride; Trazodonum [Inn-Latin]; Trazodonum [Latin]; Trazolan; Trazonil; Trialodine; Trittico | ||
| Indication | For the treatment of depression | ||
| Sponsored links | Description | Not Available | |
| Pharmacology | Trazodone is an antidepressant and hypnotic chemically unrelated to tricyclic, tetracyclic, or other known antidepressant agents. The mechanism of Trazodone's antidepressant action in man is not fully understood. In animals, Trazodone selectively inhibits serotonin uptake by brain synaptosomes and potentiates the behavioral changes induced by the serotonin precursor, 5-hydroxytryptophan. Cardiac conduction effects of Trazodone in the anesthetized dog are qualitatively dissimilar and quantitatively less pronounced than those seen with tricyclic antidepressants. Trazodone is not a monoamine oxidase inhibitor and, unlike amphetamine-type drugs, does not stimulate the central nervous system. In man, Trazodone is well absorbed after oral administration without selective localization in any tissue. Since the clearance of Trazodone from the body is sufficiently variable, in some patients Trazodone may accumulate in the plasma. | ||
| Mechanism Of Action | Trazodone binds at 5-HT2 receptor, it acts as a serotonin agonist at high doses and a serotonin antagonist at low doses. Like fluoxetine, trazodone's antidepressant activity likely results from blockage of serotonin reuptake by inhibiting serotonin reuptake pump at the presynaptic neuronal membrane. If used for long time periods, postsynaptic neuronal receptor binding sites may also be affected. The sedative effect of trazodone is likely the result of alpha-adrenergic blocking action and modest histamine blockade at H1 receptor. It weakly blocks presynaptic alpha2-adrenergic receptors and strongly inhibits postsynaptic alpha1 receptors. Trazodone does not affect the reuptake of norepinephrine or dopamine within the CNS. | ||
| Trazodone News (When available) |
Mechanic jailed for date rape of lap-dancer 17 May 2006 Policies on mentally troubled troops questioned 17 May 2006 Op-Ed Contributor Generic Smear Campaign May 10, 2006 Drug Makers Pay Doctors To Write Studies Criticizing Generic Drugs ... May 9, 2006 Clubber denies raping lapdancer after she was drugged May 11, 2006 Patient Management Exercise FOR PSYCHOTHERAPY May 15, 2006 No More Counting Sheep May 3, 2006 Innovations: Geriatric Psychiatry: Diagnosis and Treatment of ... May 10, 2006 District Court Report May 10, 2006 To Understand Depression, Look to Psychobiology, Not Biopsychiatry Apr 28, 2006 For Katrina evacuee, a life still adrift May 7, 2006 District Court May 6, 2006 Sepracor Announces First Quarter 2006 Results Apr 25, 2006 Sepracor Announces First Quarter 2006 Results Apr 25, 2006 Update on the Antidepressant Controversy Apr 17, 2006 Labopharm reports results for first quarter fiscal 2006 Apr 25, 2006 Physicians Accused of Aiding, Profiting From Drug Abusers Apr 23, 2006 | ||
| Dosage Forms | TABLET | ||
| Drug_Category | Antidepressants, Second-Generation; Anti-anxiety Agents; Serotonin Uptake Inhibitors; ATC:N06AX05 | ||
| Absorption | Well absorbed | ||
| Interactions |
-->Interactions for Trazodone: In vitro drug metabolism studies suggest that there is a potential for drug interactions when trazodone is given with CYP3A4 inhibitors. Ritonavir, a potent CYP3A4 inhibitor, increased the Cmax, AUC, and elimination half- life, and decreased clearance of trazodone after administration of ritonavir twice daily for 2 days. Adverse effects including nausea, hypotension, and syncope were observed when ritonavir and trazodone were coadministered. It is likely that ketoconazole, indinavir, and other CYP3A4 inhibitors such as itraconazole or nefazodone may lead to substantial increases in trazodone plasma concentrations, with the potential for adverse effects. If trazodone is used with a potent CYP3A4 inhibitor, a lower dose of trazodone should be considered. Carbamazepine reduced plasma concentrations of trazodone when co-administered. Patients should be closely monitored to see if there is a need for an increased dose of trazodone when taking both drugs. Increased serum digoxin or phenytoin levels have been reported to occur in patients receiving DESYREL concurrently with either of those two drugs. It is not known whether interactions will occur between mono-amine oxidase (MAO) inhibitors and DESYREL. Due to the absence of clinical experience, if MAO inhibitors are discontinued shortly before or are to be given concomitantly with DESYREL, therapy should be initiated cautiously with gradual increase in dosage until optimum response is achieved. Therapeutic Interactions Concurrent administration with electroshock therapy should be avoided because of the absence of experience in this area. There have been reports of increased and decreased prothrombin time occurring in warfarinized patients who take DESYREL. | ||
| Toxicity | LD50=96mg/kg (i.v. in mice) | ||
| Organisms Affected | Humans and other mammals | ||
| Chemical IUPAC Name | 8-[3-[4-(3-chlorophenyl)piperazin-1-yl]propyl]-6,8,9-triazabicyclo[4.3.0]nona-2,4,9-trien-7-one | ||
| Chemical Formula | C19H22ClN5O | ||
| Molecular Weight | 371.864 g/mol | ||
| Smiles String | C1CN(CCN1CCCN2C(=O)N3C=CC=CC3=N2)C4=CC(=CC=C4)Cl | ||
| Melting Point | 86-87°C | ||
| Water Solubility | Sparigly soluble | ||
| State | Solid | ||
| LogP/Hphobicity | 2.553 | ||
| Isoelectric Point | Not Available | ||
| Biotransformation | Hepatic | ||
| Half Life | 3-6 hours | ||
| Protein Binding [%] | 89-95% | ||
| RxList Link | RXlist | ||
| Sponsored links | |||
| Drug Reference |
http://www.drugs.com/cons/Trazodone.html http://www.rxlist.com/cgi/generic/traz.htm | ||
| Drug Type | Approved Drug | ||
| Accession No | APRD00533 | ||
| CAS Registry Number | 19794-93-5 | ||
| KEGG Compound ID | C07156 | ||
| PubChem ID | SID:172043 | ||
| PharmGKB ID | PA451744 | ||
| SwissProt ID | Not Available | ||
| GenBank ID | Not Available | ||
| Drug ID Number [DIN] | 2249804 |
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